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用于透皮给药的坎地沙坦西酯微乳剂:制剂、体外皮肤渗透及稳定性评估。

Candesartan cilexetil microemulsions for transdermal delivery: formulation, in-vitro skin permeation and stability assessment.

作者信息

Malakar Jadupati, Basu Aalok, Nayak Amit Kumar

机构信息

Department of Pharmaceutics, Seemanta Institute of Pharmaceutical Sciences, Mayurbhanj-757086, Odisha, India.

出版信息

Curr Drug Deliv. 2014;11(3):313-21. doi: 10.2174/1567201810666131211110517.

Abstract

The work investigates the formulation and evaluation of microemulsions containing olive oil, Tween 80 and isopropyl alcohol for transdermal candesartan cilexetil delivery. The pseudoternary phase diagram was constructed to determine composition of microemulsions. These formulated microemulsions were evaluated for in vitro skin permeation and stability. The microemulsion containing 72 % olive oil, 8 % water, 15 % Tween 80, and 5 % isopropylalcohol showed maximum viscosity of 29.54±0.32 mPas, average small droplet size of 180.90 nm, smaller polydispersity index of 0.37, zeta potential of -12.20 and maximum candesartan cilexetil permeation flux of 0.49±0.05 μg/cm2/h through excised porcine skin. The degradation of candesartan cilexetil microemulsions after 3 months storage was found low and its shelf-life was calculated as 3.92 years at room temperature.

摘要

该研究探讨了含橄榄油、吐温80和异丙醇的微乳剂用于透皮递送坎地沙坦酯的制剂配方及评价。构建了伪三元相图以确定微乳剂的组成。对这些制备的微乳剂进行了体外皮肤渗透和稳定性评价。含72%橄榄油、8%水、15%吐温80和5%异丙醇的微乳剂表现出最大粘度为29.54±0.32毫帕秒、平均小滴尺寸为180.90纳米、较小的多分散指数为0.37、ζ电位为-12.20,且通过离体猪皮的坎地沙坦酯最大渗透通量为0.49±0.05微克/平方厘米/小时。发现坎地沙坦酯微乳剂在储存3个月后的降解率较低,其在室温下的保质期计算为3.92年。

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